产品描述
D8-MMAD is a deuterated form of MMAD, which is a microtubule destroyer.
体外活性
MMAD (monomethyl Dolastatin 10) is coupled through a stable oxime ligation process to produce several nearly uniform antibody-drug conjugates (ADC) with a pharmacodynamic ratio of approximately 2.0. The resulting conjugate showed good pharmacokinetic properties and had strong in vitro cytotoxic activity against HER2 + cancer cells. Compared with ADCs prepared by cysteine alkylation after reduction of natural interchain disulfide bonds, site-based unnatural amino acid-based ADCs have higher cytotoxicity in vitro.
体内活性
The resulting antibody-drug conjugate (ADC) showed complete tumor regression in rodents. Their toxicological characteristics in rats have also been improved.
Cas No.
T10947
分子式
C41H58D8N6O6S
分子量
779.11
别名
Monomethylauristatin D D8;Monomethyl Dolastatin 10 D8;Demethyldolastatin 10 D8;D8-MMAD
储存和溶解度
DMSO:100 mg/mL (128.35 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years